# US 10,479,819 B2 · Oxyntomodulin analogue > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 10,479,819 B2 - Document ID: US10479819B2 - Status: Granted - Kind: B2 - Application number: 15/300,069 - Filed: 2015-05-28 - Published: 2017-06-29 - Granted: 2019-11-19 - Earliest claimed: 2014-09-23 - Assignees: Jiang, Xianxing - Applicants: Xianxing Jiang - Inventors: Xianxing Jiang; Yuanwen Chen - Web page: https://patentgrep.com/patent/US10479819B2 ## CPC - C07K 14/001: {by chemical synthesis} - A61K 8/64: Proteins; Peptides; Derivatives or degradation products thereof - A61K 47/542: {Carboxylic acids, e.g. a fatty acid or an amino acid} - A61P 3/04: Anorexiants; Antiobesity agents - A61P 3/10: for hyperglycaemia, e.g. antidiabetics - A61Q 19/06: for countering cellulitis - C07K 14/575: Hormones (derived from pro-opiomelanocortin, pro-enkephalin or pro-dynorphin C07K14/665, e.g. corticotropin C07K14/695) - C07K 14/605: Glucagons - A61K 38/00: Medicinal preparations containing peptides (peptides containing beta-lactam rings A61K31/00; cyclic dipeptides not having in their molecule any other peptide link than those which form their ring, e.g. piperazine-2,5-diones, A61K31/00; ergot alkaloids of the cyclic peptide type A61K31/48; containing macromolecular compounds having statistically distributed amino acid units A61K31/74; medicinal preparations containing antigens or antibodies A61K39/00; medicinal preparations characterised by the non-active ingredients, e.g. peptides as drug carriers, A61K47/00) - C07K: PEPTIDES (peptides in foodstuffs A23; obtaining protein compositions for foodstuffs, working-up proteins for foodstuffs A23J; preparations for medicinal purposes A61K; peptides containing beta-lactam rings C07D; cyclic dipeptides not having in their molecule any other peptide link than those which form their ring, e.g. piperazine-2,5-diones, C07D; ergot alkaloids of the cyclic peptide type C07D519/02; macromolecular compounds having statistically distributed amino acid units in their molecules, i.e. when the preparation does not provide for a specific; but for a random sequence of the amino acid units, homopolyamides and block copolyamides derived from amino acids C08G69/00; macromolecular products derived from proteins C08H1/00; preparation of glue or gelatine C09H; single cell proteins, enzymes C12N; genetic engineering processes for obtaining peptides C12N15/00; compositions for measuring or testing processes involving enzymes C12Q; investigation or analysis of biological material G01N33/00) - A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D) - A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS - A61Q: SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS ## Abstract Provided is an oxyntomodulin analogue. The analogue comprises GCGR and GLP-1R dual agonist activity, improved enzymolysis stability and biological activity, and no adverse reactions. The analogue can be used to prepare medication for treating hyperphagia, obesity and diabetes. ## Claims ### Claim 1 An oxyntomodulin analogue, comprising a parent peptide having the following amino acid sequence (SEQ ID NO: 29): His-Xaa2-Gln-Gly-Thr-Phe-Thr-Ser-Asp-Xaa10-Ser- Lys-Xaa13-Leu-Asp-Xaa16-Xaa17-Xaa18-Ala-Xaa20- Xaa21-Phe-Xaa23-Xaa24-Trp-Leu-Xaa27-Xaa28-Xaa29- Xaa30-Xaa31-Xaa32-Xaa33-Xaa34-Xaa35-Xaa36-Xaa37- Xaa38-Xaa39-Xaa40-COR1 wherein, R1=—OH or —NH2; Xaa2=Aib, Ser or D-Ser; Xaa10=Lys or Tyr; Xaa13=Lys or Tyr; Xaa16=Ser, Aib, Lys; Xaa17=Lys or Arg; Xaa18=Arg or Ala; Xaa20=His, Gln or Lys; Xaa21=Asp or Glu; Xaa23=IIe, Leu or Val; Xaa24=Glu or Gln; Xaa27=Met or Leu; Xaa28=Ser, Asn, Asp, or Arg; Xaa29=Ala, Gly, or Thr; Xaa30=Gly; Xaa31=Gly; Xaa32=Pro; Xaa33=Ser; Xaa34=Ser; Xaa35=Gly; Xaa36=Ala; Xaa37=Pro; Xaa38=Pro; Xaa39=Pro; and Xaa40=Ser; in the amino acid sequence of the parent peptide, at least one of Xaa10, Xaa16, Xaa17 or Xaa20 is Lys, the side chain of said at least one Lys or the Lys at position 12 is attached to a lipophilic substituent in such a way that a carboxyl group of the lipophilic substituent forms an amide bond with an amino group of a bridging group, the bridging group is attached to the parent peptide by means of a carboxy group of the amino acid residue of the bridging group which forms an amide bond with the amino group of the side chain of said at least one Lys or the Lys of the parent peptide; the bridging group is Glu-(PEG)m or Asp-(PEG)m or (PEG)m, wherein m is an integer of 2-10; and the lipophilic substituent is an acyl group selected from CH3(CH2)nCO— or HOOC(CH2)nCO—, wherein n is an integer of 10-24. ### Claim 2 (depends on 1) The oxyntomodulin analogue according to claim 1, wherein the parent peptide has an amino acid sequence of (SEQ ID NO: 29): His-Xaa2-Gln-Gly-Thr-Phe-Thr-Ser-Asp-Xaa10-Ser- Lys-Xaa13-Leu-Asp-Xaa16-Xaa17-Xaa18-Ala-Xaa20- Xaa21-Phe-Xaa23-Xaa24-Trp-Leu-Xaa27-Xaa28-Xaa29- Xaa30-Xaa31-Xaa32-Xaa33-Xaa34-Xaa35-Xaa36-Xaa37- Xaa38-Xaa39-Xaa40-COR1 wherein, R1=—NH2; Xaa2=Aib or D-Ser; Xaa10=Lys or Tyr; Xaa13=Lys or Tyr; Xaa16=Ser, Aib, or Lys; Xaa17=Lys or Arg; Xaa18=Arg or Ala; Xaa20=His, Gln or Lys; Xaa21=Asp or Glu; Xaa23=IIe or Val; Xaa24=Glu or Gln; Xaa27=Met or Leu; Xaa28=Asn, Arg, or Asp; Xaa29=Gly or Thr; Xaa30=Gly; Xaa31=Gly; Xaa32=Pro; Xaa33=Ser; Xaa34=Ser; Xaa35=Gly; Xaa36=Ala; Xaa37=Pro; Xaa38=Pro; Xaa39=Pro; and Xaa40=Ser. ### Claim 3 (depends on 1) The oxyntomodulin analogue according to claim 1, wherein that a molecular bridge is formed between the side chains of amino acid residue pairs 12 and 16, 16 and 20, 17 and 21, or 20 and 24. ### Claim 4 (depends on 2) The oxyntomodulin analogue according to claim 2, wherein the amino acid sequence of the parent peptide is a sequence selected from the group consisting of SEQ ID NO.7, SEQ ID NO.10, SEQ ID NO.13, and SEQ ID NO.17. ### Claim 5 (depends on 1) The oxyntomodulin analogue according to claim 1, wherein that-when the position 10, 12, 16, 17, or 20 of the amino acid sequence is Lys, the lipophilic substituent attached to the side chain of Lys is one of the following structures: ### Claim 6 (depends on 1) A pharmaceutical composition comprising the oxyntomodulin analogue of claim 1. ### Claim 7 (depends on 1) A method of making a drug for treating diabetes, the method comprising preparing the oxyntomodulin analogue of claim 1. ### Claim 8 (depends on 1) A method of making a drug for reducing blood glucose, the method comprising preparing the oxyntomodulin analogue of claim 1. ### Claim 9 (depends on 3) The oxyntomodulin analogue according to claim 3, wherein, when the position 16 of the amino acid sequence is Lys, the lipophilic substituent attached to the side chain of Lys is one of the following structures: ### Claim 10 (depends on 3) A pharmaceutical composition comprising the oxyntomodulin analogue of claim 3.